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Endothelium (cell layer of blood and lymphatic vessels)
01
Overview
The endothelium is a tissue layer made up of a single sheet of squamous endothelial cells lining the inner surfaces of blood vessels and lymphatic vessels. It maintains the barrier between the blood or lymph and surrounding tissues, regulates blood flow, vascular tone, hemostasis, permeability, and immune cell trafficking. Endothelial cells are dynamic, responding to mechanical and chemical signals to modulate vasodilation/constriction, inflammation, and angiogenesis[1][5][7]. Dysfunction or injury to the endothelium underlies a wide range of disease processes, including cardiovascular disease, inflammation, and cancer. While specific molecules expressed on endothelial cells can be therapeutic targets, “endothelium” as a whole should not be listed as a drug target or receptor[2][4][5].
- Other names
- endothelial cell layervascular endotheliumlymphatic endotheliumendocardium (specific to heart chambers)
02
Mechanism of action
N/A for endothelium as a cell layer
03
Biological functions
Barrier function: controls passage of materials and fluid between blood/lymph and tissuesBlood vessel tone regulation: vasodilation and vasoconstrictionHemostasis and thrombosis: regulation of clotting and anti-clotting factorsImmune response/inflammation: recruitment and signaling to immune cellsAngiogenesis: formation of new blood vesselsHormone/metabolite trafficking: interaction with growth factors, hormones, vasoactive substances
04
Disease associations
Cardiovascular disease: hypertension, atherosclerosis, thrombosis, heart diseaseInflammation: chronic inflammatory conditionsCancer: tumor angiogenesis, metastasisPulmonary disease: vascular injury, pulmonary hypertensionOther: immune dysfunction, renal disease
05
Safety considerations
Damage to or dysfunction of the endothelium leads to risk of thrombosis, hemorrhage, impaired vascular function, increased vascular permeability (edema)Targeting endothelial cells in cancer or inflammation carries risks of off-target effects, systemic vascular impact
06
Interacting drugs
drugs targeting ICAM-1, VCAM-1, PECAM-1 (monoclonal antibodies)
2 more in the full profile.
07
Biomarkers
measurement of endothelial dysfunction via flow-mediated dilationlevels of molecules like VCAM-1, ICAM-1, PECAM-1, angiopoietin-2, nitric oxide products, etc.
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